Post‐translational modifications of histones: Mechanisms, biological functions, and therapeutic targets

R Liu, J Wu, H Guo, W Yao, S Li, Y Lu, Y Jia… - MedComm, 2023 - Wiley Online Library
Histones are DNA‐binding basic proteins found in chromosomes. After the histone
translation, its amino tail undergoes various modifications, such as methylation, acetylation …

Glioblastoma: current status, emerging targets, and recent advances

A Thakur, C Faujdar, R Sharma, S Sharma… - Journal of Medicinal …, 2022 - ACS Publications
Glioblastoma (GBM) is a highly malignant brain tumor characterized by a heterogeneous
population of genetically unstable and highly infiltrative cells that are resistant to …

Histone lysine demethylases as targets for anticancer therapy

JW Højfeldt, K Agger, K Helin - Nature reviews Drug discovery, 2013 - nature.com
It has recently been demonstrated that the genes controlling the epigenetic programmes that
are required for maintaining chromatin structure and cell identity include genes that drive …

The histone demethylase KDM1A sustains the oncogenic potential of MLL-AF9 leukemia stem cells

WJ Harris, X Huang, JT Lynch, GJ Spencer, JR Hitchin… - Cancer cell, 2012 - cell.com
Using a mouse model of human MLL-AF9 leukemia, we identified the lysine-specific
demethylase KDM1A (LSD1 or AOF2) as an essential regulator of leukemia stem cell (LSC) …

Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells

W Fiskus, S Sharma, B Shah, BP Portier, SGT Devaraj… - Leukemia, 2014 - nature.com
The histone demethylase LSD1 (KDM1A) demethylates mono-and di-methylated (Me2)
lysine (K) 4 on histone H3. High LSD1 expression blocks differentiation and confers a poor …

[HTML][HTML] Long non-coding RNA HOTAIR promotes glioblastoma cell cycle progression in an EZH2 dependent manner

K Zhang, X Sun, X Zhou, L Han, L Chen, Z Shi… - Oncotarget, 2015 - ncbi.nlm.nih.gov
The long non-coding RNA Hox transcript antisense intergenic RNA (HOTAIR) was recently
implicated in breast cancer metastasis and is predictive of poor prognosis in colorectal and …

Re-programing chromatin with a bifunctional LSD1/HDAC inhibitor induces therapeutic differentiation in DIPG

JN Anastas, BM Zee, JH Kalin, M Kim, R Guo… - Cancer cell, 2019 - cell.com
Summary H3K27M mutations resulting in epigenetic dysfunction are frequently observed in
diffuse intrinsic pontine glioma (DIPGs), an incurable pediatric cancer. We conduct a …

Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors

AKA Bass, MS El-Zoghbi, ESM Nageeb… - European journal of …, 2021 - Elsevier
Despite the encouraging clinical progress of chemotherapeutic agents in cancer treatment,
innovation and development of new effective anticancer candidates still represents a …

Epidrug repurposing: discovering new faces of old acquaintances in cancer therapy

M Montalvo-Casimiro, R González-Barrios… - Frontiers in …, 2020 - frontiersin.org
Gene mutations are strongly associated with tumor progression and are well known in
cancer development. However, recently discovered epigenetic alterations have shown the …

LSD1-directed therapy affects glioblastoma tumorigenicity by deregulating the protective ATF4-dependent integrated stress response

S Faletti, D Osti, E Ceccacci, C Richichi… - Science Translational …, 2021 - science.org
Glioblastoma (GBM) is a fatal tumor whose aggressiveness, heterogeneity, poor blood-brain
barrier penetration, and resistance to therapy highlight the need for new targets and clinical …